Assay Detail
Binding
CHEMBL891766
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [N-methyl-3H]GW0438X from human PXR
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.34 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430006 | — | — | 1 | 7.70 |
| CHEMBL396952 | — | — | 1 | 7.60 |
| CHEMBL62136 | T091317 | — | 1 | 7.40 |
| CHEMBL242293 | — | — | 1 | 7.20 |
| CHEMBL388024 | — | — | 1 | 6.60 |
| CHEMBL242528 | — | — | 1 | 6.50 |
| CHEMBL396953 | — | — | 1 | 6.20 |
| CHEMBL242291 | — | — | 1 | 5.80 |
| CHEMBL396041 | — | — | 1 | 5.60 |
| CHEMBL242527 | — | — | 1 | 5.40 |
| CHEMBL389979 | — | — | 1 | 5.10 |
| CHEMBL242526 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430006 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL396952 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL62136 | T091317 | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL242293 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL388024 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL242528 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL396953 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL242291 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL396041 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL242527 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL389979 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL242526 | — | IC50 | = | 10000.0 | nM | 5.00 |